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UCD SF I Dosage Forms
Dr. Jones Braun's lectures
134
Other
Professional
09/29/2010

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Term
What dictates drug dosage form?
Definition
Drug Potency
Term
What can influence patient compliance?
Definition
Convenient or agreeable dosage forms
Term
Low molecular weight salts would have what predicted taste sensation?
Definition
Salty
Term
High molecular weight salts would have what predicted taste sensation?
Definition
Bitter
Term
What taste sensation results from increased hydroxyl groups?
Definition
Sweet
Term
What taste sensation do plant alkyloids produce?
Definition
Bitter
Term
What is taste masking used for?
Definition
Concealing bitter, salty or otherwise offensive tastes and odors.
Term
Modes of local drug delivery?
Definition
Aerosols, ointments, nasal sprays, vaginal products
Term
When taken orally drugs absorbed in the GI tract pass through ______?
Definition
The Liver
Term
What effect does the liver have on drugs absorbed from the GI tract?
Definition
Decreased systemic concentrations
Term
What are advantages of delayed onset dosage forms?
Definition
Dosage delivered at a time later then when it is taken. Drug released hours after taken to coincide with natural biorhythms
Term
Advantages of Sustained Release dosage forms?
Definition
Maintain therapeutic concentrations, decrease dosing frequency, increase patient compliance.
Term
Advantages of Modified Release dosage forms?
Definition
Different dosages delivered throughout the day.
Term
Advantage of Pulsatile Release dosage form?
Definition
Dose delivered multiple times through the day.
Term
Functional Groups that are susceptible to hydrolysis?
Definition
Esters, substituted amides, lactones, lactams
Term
How can drugs be protected from hydrolysis?
Definition
Film coating, low humidity storage, Substitute water, reconstitute immediately prior to administration, store in cool spot
Term
Drugs vulnerable to oxidation?
Definition
Aldehydes,alcohols, phenols, sugars, alkaloids, fats/oils
Term
When does oxidation usually occur?
Definition
In presence of water, trace metals, or when exposed to light
Term
Color changes, odors and precipitants are signs of __________?
Definition
Oxidation
Term
What can be done to protect drugs from oxidation?
Definition
Antioxidants, Store in inert gas, Chelate metals, protect from light, store in cool place
Term
Define High solubility.
Definition
Drug whose highest strength is soluble in <250 mL of water with a pH range of 1-7.5
Term
Define high permeablity
Definition
A drug with an extent of absorption >90% of the administered dose.
Term
What does Lipinski's Rule of 5 predict?
Definition
Poor permeability
Term
Advantages of oral dosage forms?
Definition
good patient compliance, good stability, can alter dissolution profile, easy to dispense
Term
Types of oral dosage forms?
Definition
Tablets, Capsules, chewing gum, liquids
Term
Most common oral dosage form?
Definition
Compressed Tablet
Term
Purpose of excipients in tablets?
Definition
Promote disintegration, improve feel in mouth, improve flow, improve compression, ease of formulation
Term
Purpose of binders and granulators?
Definition
Promote adhesion, maintain tablet integrity, determine hardness
Term
The hardness of chewable tablets is ___, the hardness of nonchewable tablets are ____, the hardness of sustained release tablets are ___.
Definition
3, 4-10, 10-20
Term
Advantages of rectal dosage forms
Definition
Circumvent 1st pass metabolism, good for GI irritants, less hostile environment for drugs
Term
Disadvantages of rectal dosage forms.
Definition
Irregular absorbtion, inconvenient, leakage or expulsion after insertion.
Term
Water based suppositories release ______ drugs best, where fat based suppositories release _________ drugs best.
Definition
fat soluble, water soluble
Term
How many mLs can be injected intramuscularly?
Definition
2mL Deltoid, 5mL Gluteal
Term
Volume limit for subcutaneous administration
Definition
1.3 mL
Term
Advantage of intravenous administration
Definition
rapid onset
Term
Advantages of intramuscular administration.
Definition
slower onset, longer duration
Term
advantages of subcutaneous administration
Definition
slowest onset, long duration
Term
Use of parenteral administration?
Definition
Local or systemic action
Term
Advantages of parenteral administration
Definition
good for drugs inactivated in GI tract, rapid onset, good for pts that cant take oral meds, circumvents 1st pass metabolism
Term
Transdermal dose relates to ?
Definition
SA of skin, duration of contact, permeability through skin
Term
Advantages of transdermal administration?
Definition
Avoids GI absorption problems, can substitute for oral form, Circumvent 1st pass metabolism, painless, terminate drug effect easily
Term
Advantages of pulmonary routes of administration.
Definition
High concentration delivered locally, circumvent 1st pass metabolism, good for drugs inactivated in GI tract
Term
Concerns with ocular administration?
Definition
Osmolarity, tonicity, pH, sterility
Term
Define dissolution
Definition
Change in phase from solid to liquid
Term
What is absorption?
Definition
Movement of dissolved drug from liquid to blood
Term
Rate limiting step is ?
Definition
The slowest step in a process
Term
Factors that determine effectiveness of dosage form
Definition
disintegration rate, deaggregation rate, rate of dissolution
Term
What does the Noyes & Whitney equation deal with?
Definition
dissolution
Term
Noyes & Whitney equation is _____?
Definition
dM/dt = DS (Cs - C) / h
Term
What does the term dM/dt signify?
Definition
change in mass/change in time
Term
What does the term D in the N&W equation signify?
Definition
diffusion coefficient of solute
Term
What does the term S in the N&W equation signify?
Definition
Surface are of drug
Term
What does the term Cs in the N&W equation signify?
Definition
Max solubility of drug
Term
What does the term C in the N&W equation signify?
Definition
Concentration of drug in solvent
Term
What does the term h in the N&W equation signify?
Definition
thickness of diffusion layer
Term
how to increase diffusion coefficient (D)
Definition
decrease viscosity, increase solvent temp
Term
How to increase Surface Area of drug (S)
Definition
make particle size smaller
Term
How to make particle sizes smaller
Definition
Chew, crush, cut, micronize, nanocrystalize, mortar and pestle
Term
how to decrease diffusion layer
Definition
mix with effervescent salts
Term
How to increase solubility of drug
Definition
Salt form, crystalline form, prodrug, solvent pH
Term
What dissolves faster, Free acid or sodium/potassium salt, regardless of dissolution media pH.
Definition
Sodium/Potassium Salt
Term
What is polymorphism
Definition
When more then one crystalline form is possible
Term
What is a metastable form?
Definition
a polymorphic form that converts to the stable crystalline form.
Term
Do polymorphic forms have the same physical and chemical properties?
Definition
No
Term
Which has higher solubility and bioavailable, the stable crystalline form or the Metastable form.
Definition
Metastable form
Term
Do amorphous forms exhibit crystallinity?
Definition
No
Term
What is more stable, Crystal form or amorphous form.
Definition
Crystal Form
Term
Amorphous form is ________ to chemical degradation than the crystalline form
Definition
more resistant
Term
Which uses more energy to dissolve, Amorphous form or Crystalline form.
Definition
Crystalline form
Term
Absorption
Definition
Movement of drug into blood stream
Term
4 factors affecting drug absorption
Definition
physiochemical properties, formulations, route of administration, the patient
Term
What are the physiochemical properties that affect absorption
Definition
molecular weight, ionization state, hydrophobicity,structure
Term
Can you predict drug absorption characteristics from several homologous drugs that only vary by one physiochemical property each?
Definition
yes
Term
What does drug absorption usually rely on?
Definition
Crossing a membrane to reach the blood stream.
Term
Physiochemical factors that affect absorption.
Definition
binding to transporter, hydrophobic, low molecular weight, and non-ionized state
Term
Formulation factors that affect drug absorption.
Definition
Dosage form, prodrug, excipients
Term
What is ADME
Definition
Absorption, distribution, metabolism, elimination
Term
Prodrugs are designed to affect what?
Definition
ADME
Term
Do IV drugs have to cross a membrane to be effective?
Definition
No, they are already in the blood stream.
Term
primary component of cell membrane
Definition
lipids
Term
Define paracellular
Definition
movement between cells
Term
define transcellular
Definition
movement through cells
Term
Is transcellular movement active or passive diffusion?
Definition
Passive diffusion
Term
in transcellular, passive diffusion what determines the diffusion rate?
Definition
Concentration, size, lipid solubility, absorptive surface area, and ionization state
Term
in which direction can active transport move substances, with regard to concentration gradient?
Definition
Against the concentration gradient
Term
is energy required in active transport?
Definition
yes
Term
is energy required for facilitated passive diffusion?
Definition
no
Term
can facilitated passive diffusion transport against the concentration gradient?
Definition
no
Term
is energy required for receptor mediated transport?
Definition
yes
Term
for which type of drugs is receptor mediated transport useful.
Definition
Protein based drugs
Term
What patient factors affect drug absorption?
Definition
Age, sex, health, and nutritional state
Term
Age factors affecting drug absorption
Definition
Skin thickness, stomach acidity
Term
What are the three types of dispersions?
Definition
True, colloidial, Coarse
Term
define a true dispersion
Definition
< 1nm phase dispersion
Term
define colloidal dispersion
Definition
1-500 nm phase dispersion
Term
define coarse dispersion
Definition
0.5 micrometers to 50 micrometers phase dispersion
Term
Define surface tension
Definition
Force per unit area applied parallel to to the surface in order to counterbalance the net inward pull
Term
The higher the the surface tension, the _______ the energy stored at the interface.
Definition
Higher
Term
What does Wa indicate?
Definition
Work of adhesion
Term
What does Wc indicate
Definition
work of cohesion
Term
What does S indicate in S=Wa-Wc?
Definition
Spreading coefficient
Term
Spreading occurs when?
Definition
adhesion forces are greater then cohesion forces
Term
When S is positive spreading ________?
Definition
occurs (Wa-Wc>0)
Term
What determines if a droplet will spread?
Definition
reduction in surface free energy
Term
What type of characteristics do surfactants have?
Definition
both hydrophobic and hydrophillic
Term
Surfactants are ___________?
Definition
Surface active Agents
Term
Surfactants help orient hydrophobic moieties toward which phase?
Definition
the oily phase
Term
What can colloidal dispersions be viewed with?
Definition
ultramicroscope, electron microscope
Term
Colloidal dispersions have _____ diffusion
Definition
slow
Term
define sols
Definition
fluid, lower viscosity then gels
Term
define gels
Definition
solid particles form bridged particles with mechanical strength
Term
what designates the dispersion vehicle?
Definition
the prefix ex. hydrogel, alcogel, aerogel
Term
define lyophilic
Definition
Solvent loving
Term
define lyophobic
Definition
solvent hating
Term
Extensive solvation of the dispersed phase
Definition
lyophilic dispersion
Term
dispersed phase has strong affinity for oils
Definition
lyophilic
Term
What type of vehicle is usually associated with lyophilic dispersions?
Definition
nonpolar liquid heavy in hydrocarbons and low dielectric constant
Term
Dispersion that has little attraction between particle and vehicle
Definition
lyophobic
Term
Dispersed phase consisting of aggregate of molecules too small to be considered colloid.
Definition
Association colloid
Term
define amphiphillic
Definition
Having large hydrophobic and hydrophilic groups on same molecule
Term
What does the equation D=RT/6(pi)nrN
Definition
Diffusion coefficient for spherical molecules
Term
What does R indicate in D=RT/6(pi)nrN
Definition
Gas Constant
Term
What does T indicate in D=RT/6(pi)nrN
Definition
Absolute temperature
Term
What does n indicate in D=RT/6(pi)nrN
Definition
vehicle viscosity
Term
What does r indicate in D=RT/6(pi)nrN
Definition
particle radius
Term
What does N indicate in D=RT/6(pi)nrN
Definition
Avogadro's number
Term
What governs particle movement in dispersions?
Definition
Brownian motion. x=sqrt(2Dt)
Term
Dissolution rates and absorption are affected by _______?
Definition
Particle size
Term
What causes particle size to increase?
Definition
sedimentation or creaming
Term
Properties of Emulsions
Definition
two or more immiscible fluids, 0.1-100nm, does not separate easily
Term
What is HLB
Definition
Hydrophile-Lipophile Balance
Term
High HLB indicates
Definition
more hydrophilic
Term
Low HLB indcates
Definition
more hydrophobic
Term
Advantages of Suspensions
Definition
easier to swallow, flexible dosing, more palatable taste, prolonged therapeutic effect, deliver poor water soluble drugs
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